title: Lipopeptide with a RGDK tetrapeptide sequence can selectively target genes to proangiogenic alpha5beta1 integrin receptor and mouse tumor vasculature.
abstract: Integrins, the major class of alphabeta heterodimeric transmembrane glycoprotein receptors, play crucial roles in mediating tumor angiogenesis. Genetic ablation experiments combined with use of antibodies/peptide ligands for blocking either alpha(5) or beta(1) integrins have convincingly demonstrated alpha(5)beta(1) integrin to be unquestionably proangiogenic among the 24 known integrin receptors. Herein, we report on a novel RGDK-lipopeptide 1 that targets selectively alpha(5)beta(1) integrin and is capable of targeting genes to mouse tumor vasculatures.
authors.affiliation: Division of Lipid Science and Technology, Pharmacology Division, Indian Institute of Chemical Technology, Hyderabad 500607, India.
authors.forename: Dipankar
authors.initials: D
authors.lastname: Pramanik
authors.forename: Bharat K
authors.initials: BK
authors.lastname: Majeti
authors.forename: Goutam
authors.initials: G
authors.lastname: Mondal
authors.forename: Priya P
authors.initials: PP
authors.lastname: Karmali
authors.forename: Ramakrishna
authors.initials: R
authors.lastname: Sistla
authors.forename: Obula G
authors.initials: OG
authors.lastname: Ramprasad
authors.forename: Gunda
authors.initials: G
authors.lastname: Srinivas
authors.forename: Gopal
authors.initials: G
authors.lastname: Pande
authors.forename: Arabinda
authors.initials: A
authors.lastname: Chaudhuri
mesh_terms: D000818:Animals; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D039081:Integrin alpha5beta1 / Q000037:antagonists & inhibitors* / Q000235:genetics* / Q000378:metabolism; D055666:Lipopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D009389:Neovascularization, Pathologic / Q000188:drug therapy / Q000235:genetics*
chemical_list: D039081:Integrin alpha5beta1; D055666:Lipopeptides